青岛大学学报（医学版）2025，Vol.61Issue(6)：813-819,7.DOI:10.11712/jms.2096-5532.2025.61.191
西地那非口崩片在中国健康受试者中的生物等效性
Bioequivalence of sildenafil citrate orally disintegrating tablets in healthy Chinese subjects
摘要
Abstract
Objective To investigate the bioequivalence of the test and reference products of sildenafil citrate orally disinte-grating tablets in healthy Chinese subjects in a fasting state.Methods This single-center,randomized,open-label,two-treat-ment,two-sequence,two-period,crossover study was conducted among 36 healthy adult male subjects.The subjects received the test product or the reference product of sildenafil citrate orally disintegrating tablets at a dose of 50 mg in each period,with a 5-day washout between treatments.A validated high-performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS)method was used to measure the plasma concentrations of sildenafil and its major metabolite N-desmethyl sildenafil.The non-com-partmental analysis was performed for plasma concentration data.Phoenix WinNonlin 8.2 was used to calculate pharmacokinetic pa-rameters,and SAS 9.4 was used to perform bioequivalence analysis.Results After the administration of the test and reference products,the peak concentration(Cmax)of sildenafil was 252.00±104.00 μg/L and 255.00±90.70 μg/L,respectively,with an area under the plasma concentration-time curve from time 0 to the time of last measurement(AUC0-t)of 694.41±269.29 μg·h/L and 687.71±247.19 μg·h/L,respectively,and an area under the plasma concentration-time curve from time 0 extrapolated to in-finity(AUC0-∞)of 705.21±272.18 μg·h/L and 699.43±251.85 μg·h/L,respectively.The Cmax of N-desmethyl sildenafil was 94.00±32.70 μg/L and 96.10±38.80 μg/L,respectively,with an AUC0-t of 322.52±121.29 μg·h/L and 331.33±145.82 μg·h/L,respectively,and an AUC0-∞ of 333.93±127.15 μg·h/L and 345.09±159.03 μg·h/L,respectively.The geometric mean ra-tios of Cmax,AUC0-t,and AUC0-∞ for the two formulations of sildenafil were 97.36％(95％CI=89.03％-106.47％),100.18％(95％CI=96.57％-103.92％),and 100.08％(95％CI=96.51％-103.77％),respectively,and the geometric mean ratios of Cmax,AUC0-t,and AUC0-∞ for the two formulations of N-desmethyl sildenafil were 98.84％(95％CI=92.14％-106.25％),98.54％(95％CI=95.87％-101.28％),and 98.23％(95％CI=95.45％-101.09％),respectively.All these results were within the bioequivalence acceptance range of 80.00％—125.00％.Con-clusion The test and reference products of sildenafil citrate orally disintegrating tablets are bioequivalent in healthy Chinese sub-jects,with a good safety profile.关键词
枸橼酸西地那非/药代动力学/生物等效性/血药浓度/健康受试者Key words
sildenafil citrate/pharmacokinetics/bioequivalency/plasma concentration/healthy volunteers分类
医药卫生引用本文复制引用
周雨石,秦如斋,易德平,林金水,陈学义,谢志红..西地那非口崩片在中国健康受试者中的生物等效性[J].青岛大学学报（医学版）,2025,61(6):813-819,7.基金项目
广东省医学科学技术研究基金(B2023146) （B2023146）
